AFDX-384 explained

AFDX-384 (BIBN-161) is a drug which acts as a selective antagonist of the muscarinic acetylcholine receptors, with selectivity for the M₂ and M₄ subtypes. It is used mainly for mapping the distribution of M₂ and M₄ muscarinic receptors in the brain, and studying their involvement in the development and treatment of dementia and schizophrenia.^{[1] [2] [3] [4] [5] [6] [7]}

See also

• Pirenzepine (M₁ selective antagonist)

Notes and References

1. Tränkle C, Andresen I, Lambrecht G, Mohr K . M2 receptor binding of the selective antagonist AF-DX 384: possible involvement of the common allosteric site . Molecular Pharmacology . 53 . 2 . 304–12 . February 1998 . 9463489 . 10.1124/mol.53.2.304.
2. Kitaichi K, Day JC, Quirion R . A novel muscarinic M(4) receptor antagonist provides further evidence of an autoreceptor role for the muscarinic M(2) receptor sub-type . European Journal of Pharmacology . 383 . 1 . 53–6 . October 1999 . 10556681 . 10.1016/S0014-2999(99)00607-X.
3. Martin J, Deagostino A, Perrio C, Dauphin F, Ducandas C, Morin C, Desbène PL, Lasne MC . Syntheses of R and S isomers of AF-DX 384, a selective antagonist of muscarinic M2 receptors . Bioorganic & Medicinal Chemistry . 8 . 3 . 591–600 . March 2000 . 10732976 . 10.1016/S0968-0896(99)00307-7.
4. Piggott M, Owens J, O'Brien J, Paling S, Wyper D, Fenwick J, Johnson M, Perry R, Perry E . Comparative distribution of binding of the muscarinic receptor ligands pirenzepine, AF-DX 384, (R,R)-I-QNB and (R,S)-I-QNB to human brain . Journal of Chemical Neuroanatomy . 24 . 3 . 211–23 . September 2002 . 12297267 . 10.1016/S0891-0618(02)00066-2. 1935197 .
5. Zavitsanou K, Katsifis A, Yu Y, Huang XF . M2/M4 muscarinic receptor binding in the anterior cingulate cortex in schizophrenia and mood disorders . Brain Research Bulletin . 65 . 5 . 397–403 . May 2005 . 15833594 . 10.1016/j.brainresbull.2005.02.007 . 19527958 .
6. Teaktong T, Piggott MA, Mckeith IG, Perry RH, Ballard CG, Perry EK . Muscarinic M2 and M4 receptors in anterior cingulate cortex: relation to neuropsychiatric symptoms in dementia with Lewy bodies . Behavioural Brain Research . 161 . 2 . 299–305 . June 2005 . 15922057 . 10.1016/j.bbr.2005.02.019 . 34247659 .
7. Gibbons AS, Scarr E, McLean C, Sundram S, Dean B . Decreased muscarinic receptor binding in the frontal cortex of bipolar disorder and major depressive disorder subjects . Journal of Affective Disorders . 116 . 3 . 184–91 . August 2009 . 19103464 . 2724602 . 10.1016/j.jad.2008.11.015 .